Biological Information
Background Information:
Adrenoreceptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Adrenoreceptors are found in most peripheral tissue and within the central nervous system.
Family:
GPCR
Sub Family:
Adrenoceptor
Class:
Class A
Protein Name:
alpha1D
Uniprot Number:
P25100
Protein Aliases:
Alpha-1D adrenoreceptor|Alpha-1D adrenoceptor|Alpha-adrenergic receptor 1a
Gene Name:
ADRA1D
Gene ID:
146
Gene Aliases:
ADRA1R|ADRA1A|ADRA1
Accession Number:
NM_000678
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
HEK293
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
1 hr at 37°C
Control Inhibitor:
Bmy-7378
Criteria For Significance:
≥ 50% increase in IP-one relative to Phenylephrine response, ≥ 50% Inhibition of Phenylephrine-induced response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Adverse / Beneficial Action:
Adrenergic a1D receptor antagonism may be useful in the treatment of hypertension with minimal associated orthostatic hypotension.
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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